The concept of radiolabelled peptide analogues to target cell membrane-bound receptors is subject of an increasing number of research projects and source of inspiration for many researchers throughout the world. The first application of radiolabelled peptides in the human was introduced by Krenning et al. in 1989. The somatostatin analogue Tyr3-octreotide was labelled with 123I and scintigraphy to localise somatostatin receptor positive tumours was established. However, the use of 123I-Tyr3-octreotide for scintigraphy had several major drawbacks regarding its metabolic behaviour, preparation difficulties and the relatively short physical half-life of the radionuclide. Therefore, another radiolabelled analogue of somatostatin, 111In-DTPA-D-Phe1-octreotide was introduced which had several advantages such as easy preparation, general availability, appropriate half-life and absence of major interference in the upper abdominal region. In 1994, 111In-DTPA-D-Phe1-octreotide (OctreoScan(R)) was approved by the U.S. Food and Drug Administration (FDA) and since then OctreoScan(R) has become a commonly used imaging technique to diagnose neuroendocrine tumours, such as carcinoids and neuroendocrine tumours of the pancreas. These tumours have a high expression of somatostatin receptors, especially the receptor subtype in common.

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Erasmus University Rotterdam
Erasmus MC: University Medical Center Rotterdam

Teunissen, J. (2008, December 10). Endocrine Tumours - Molecular Radiation on Target Peptide Receptor Radionuclide Therapy with Lutetium-octreotate. Retrieved from